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    • 1. 发明公开
    • Therapeutic preparations
    • 治疗方法
    • EP0284174A1
    • 1988-09-28
    • EP88300281.8
    • 1988-01-14
    • IMPERIAL CHEMICAL INDUSTRIES PLCICI PHARMA
    • Bruneau, Pierre Andre RaymondCarey, FrankDelvare, Christian Robert ErnestGibson, Keith HopkinsonMcMillan, Rodger Martin
    • C07D231/56C07D401/06C07D405/06C07D409/06C07D401/10C07D403/06C07D417/06C07D403/12C07D405/12C07D401/12C07D413/06
    • C07D231/56C07D401/06C07D401/10C07D401/12C07D403/06C07D403/12C07D405/06C07D405/12C07D409/06C07D413/06C07D417/06
    • The invention concerns pharmaceutical compositions containing a 1,2-dihydro-3 H -indazol-3-one derivative of the formula I
      wherein Ra is hydrogen, halogeno, nitro, hydroxy, (2-6C)alkanoyloxy, (1-6C)alkyl, (1-6C)alkoxy, fluoro-(1-4C)alkyl, (2-6C)alkanoyl, amino, (1-6C)alkylamino, di-[(1-4C)alkyl]amino, (2-6C)alkanoylamino or hydroxy-­(1-6C)alkyl; Rb is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; and Y is a group of the formula -A¹-X-A²-Q in which A¹ is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene, or A¹ is phenylene; X is oxy, thio, sulphinyl, sulphonyl, imino, (1-­6C)alkylimino, (1-6C)alkanoylimino, iminocarbonyl or phenylene, or X is a direct link to A²; A² is (1-6C)alkylene, (3-6C)alkenylene or (3-­6C)alkynylene or A² is cyclo(3-6C)alkylene or is a direct link to Q, or the group A¹-X-A² is a direct link to Q; or Y is (2-10)alkyl, (3-­10C)alkenyl or (3-6C)alkynyl; and Q is aryl or heteroaryl.
      The invention also provides novel 1,2-dihydro-3 H -indazol-3-­ones, processes for their production and the use of 1,2-dihydro-3 H -­indazol-3-one for the manufacture of medicaments for the treatment of various allergic and inflammatory diseases.
    • 本发明涉及含有式I 的1,2-二氢-3H-吲唑-3-酮衍生物的药物组合物,其中R a是氢,卤素,硝基,羟基,(2-6C)烷酰氧基,(1-6C )(1-6C)烷氧基,氟 - (1-4C)烷基,(2-6C)烷酰基,氨基,(1-6C)烷基氨基,二 - [(1-4C) 6C)烷酰基氨基或羟基 - (1-6C)烷基; Rb是氢,卤代,(1-6C)烷基或(1-6C)烷氧基; 并且Y是式-A 1 -XA 2 -Q的基团,其中A 1是(1-6C)亚烷基,(3-6C)亚烯基,(3-6C)亚炔基或环( 3-6C)亚烷基,或A 1是亚苯基; X是氧基,硫基,亚磺酰基,磺酰基,亚氨基,(1-6C)烷基亚氨基,(1-6C)烷酰基亚氨基,亚氨基羰基或亚苯基,或X是与A 2的直接连接。 A 2是(1-6C)亚烷基,(3-6C)亚烯基或(3-6C)亚炔基或A 2是环(3-6C)亚烷基或与Q直接相连,或基团A <1> -XA <2>是与Q的直接链接; 或Y为(2-10)烷基,(3-10C)烯基或(3-6C)炔基; Q是芳基或杂芳基。 本发明还提供新的1,2-二氢-3H-吲唑-3-酮,其制备方法和1,2-二氢-3H-吲唑-3-酮用于制备用于治疗各种药物的药物 过敏性和炎性疾病。